| Identification | Back Directory | [Name]
Indinavir sulfate | [CAS]
157810-81-6 | [Synonyms]
IDV
MK-639
CRIXIVAN
MK-639,Crixivan
INDINAVIR SULFATE
INDINAVIR SULPHATE
INDIGOWOADROOTEXTRACT
Indinavir sulfate ethanolate
Indinavir & Indinavir Sulfate
Indinavir sulfate###Unii-9mg78X43zt
indinavirsulfate(subjecttopatentfree)
2,3,5-Trideoxy-N-[(1S,2R)-2,3-dihydro-2-hydroxy-1H-inden-1-yl]-5-[(2S)-2[[(1,1-dimethylethyl)amino]carbonyl]-4-(3-pyridinylmethyl)-1-piperazinyl]-2-(phenylmethyl)-D-erythro-pentonamide
(1(1s,2r),5(s))-2,3,5-trideoxy-n-(2,3-dihydro-2-hydroxy-1h-inden-1-yl)-5-(2-(((1,1-dimethylethyl)amino)carbonyl)-4-(3-pyridinylmethyl)-1-piperazinyl)-2-(phenylmethyl)-d-erythro-pentonamide sulfate | [EINECS(EC#)]
682-418-9 | [Molecular Formula]
C36H49N5O8S | [MDL Number]
MFCD00920346 | [MOL File]
157810-81-6.mol | [Molecular Weight]
711.87 |
| Chemical Properties | Back Directory | [Appearance]
Crystalline Solid | [Melting point ]
150-153°C (dec) | [storage temp. ]
-20°C Freezer | [solubility ]
Freely soluble in water, soluble in methanol, practically insoluble in heptane. | [form ]
Solid | [color ]
White to Off-White | [Water Solubility ]
>100g/L(temperature not stated) | [BCS Class]
2,4 |
| Hazard Information | Back Directory | [Chemical Properties]
Crystalline Solid | [Uses]
Member of the novel hydroxyaminopentane amide class of HIV-1 protease inhibitors. Antiviral | [Hazard]
Moderately toxic by ingestion. | [Description]
Indinavir is an HIV-1 protease inhibitor (Ki = 0.358 nM).1 It is selective for HIV-1 protease over HIV-2 protease (Ki = 3.316 nM), as well as human cathepsin D, porcine pepsin, bovine chymosin, human plasma renin, Factor Xa, and elastase at 10 μM. It is also selective for wild-type HIV-1 protease over the protease inhibitor-resistant mutants A-44, K-60, and V-18 (Kis = 0.24, 15, 50, and 40 nM, respectively).2 Indinavir is active against multiple HIV-1 variants in cell-based assays (IC95s = 12-100 nM).1 Formulations containing indinavir have been used in combination with antiretroviral agents in the treatment of HIV infection. | [Definition]
ChEBI: Indinavir sulfate is an azaheterocycle sulfate salt. It is functionally related to an indinavir. | [Brand name]
Crixivan (Merck). | [storage]
RT | [References]
[1] J P VACCA. L-735,524: an orally bioavailable human immunodeficiency virus type 1 protease inhibitor.[J]. Proceedings of the National Academy of Sciences of the United States of America, 1994, 91 9: 4096-4100. DOI: 10.1073/pnas.91.9.4096
[2] BRUCE D. DORSEY. Identification of MK-944a: A Second Clinical Candidate from the Hydroxylaminepentanamide Isostere Series of HIV Protease Inhibitors[J]. Journal of Medicinal Chemistry, 2000, 43 18: 3386-3399. DOI: 10.1021/jm9903848 |
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